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Title: Positron emitter labeled enzyme inhibitors

Abstract

This invention involved a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide in activators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography. 2 figs.

Inventors:
; ;
Issue Date:
Research Org.:
Brookhaven National Lab., Upton, NY (USA)
OSTI Identifier:
6864415
Patent Number(s):
-US-A6052921
Assignee:
TIC; EDB-88-179699
DOE Contract Number:  
AC02-76CH00016
Resource Type:
Patent
Resource Relation:
Other Information: Portions of this document are illegible in microfiche products
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; AMINE OXIDASES; ENZYME INHIBITORS; ENZYME ACTIVITY; DISTRIBUTION; LABELLING; CARBON 11; CHEMICAL PREPARATION; INVENTIONS; ORGANIC COMPOUNDS; POSITRON COMPUTED TOMOGRAPHY; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; CARBON ISOTOPES; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; EMISSION COMPUTED TOMOGRAPHY; ENZYMES; EVEN-ODD NUCLEI; ISOTOPES; LIGHT NUCLEI; MINUTES LIVING RADIOISOTOPES; NUCLEI; OXIDOREDUCTASES; RADIOISOTOPES; SYNTHESIS; TOMOGRAPHY; 550201* - Biochemistry- Tracer Techniques; 550200 - Biochemistry

Citation Formats

Fowler, J S, MacGregor, R R, and Wolf, A P. Positron emitter labeled enzyme inhibitors. United States: N. p., 1987. Web.
Fowler, J S, MacGregor, R R, & Wolf, A P. Positron emitter labeled enzyme inhibitors. United States.
Fowler, J S, MacGregor, R R, and Wolf, A P. Fri . "Positron emitter labeled enzyme inhibitors". United States.
@article{osti_6864415,
title = {Positron emitter labeled enzyme inhibitors},
author = {Fowler, J S and MacGregor, R R and Wolf, A P},
abstractNote = {This invention involved a new strategy for imaging and mapping enzyme activity in the living human and animal body using positron emitter-labeled suicide enzyme inactivators or inhibitors which become covalently bound to the enzyme as a result of enzymatic catalysis. Two such suicide in activators for monoamine oxidase have been labeled with carbon-11 and used to map the enzyme subtypes in the living human and animal body using PET. By using positron emission tomography to image the distribution of radioactivity produced by the body penetrating radiation emitted by carbon-11, a map of functionally active monoamine oxidase activity is obtained. Clorgyline and L-deprenyl are suicide enzyme inhibitors and irreversibly inhibit monoamine oxidase. When these inhibitors are labeled with carbon-11 they provide selective probes for monoamine oxidase localization and reactivity in vivo using positron emission tomography. 2 figs.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1987},
month = {5}
}